专利号:US-8269001-B2 优先权日:2005-10-05 标题 :Process for the synthesis of HMG-CoA reductase inhibitors 发明人:CASAR ZDENKO 权利人:CASAR ZDENKO; LEK PHARMACEUTICALS 摘要:A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.
专利号:US-2023220001-A1 优先权日:2020-06-09 标 题:Method for synthesis of thioether-containing peptides 发明人:GRUSS HENDRIK; LUTZ CHRISTIAN; SÜSSMUTH RODERICH; Yao guiyang; KNITTEL CAROLINE; KOSOL SIMONE; MAINZ ANDI 权利人:HEIDELBERG PHARMA RES GMBH 摘要:The present invention relates to a method of formation of a sulphur bridge between tryptophan and cysteine in solid phase peptide synthesis under iodine treatment. The invention also relates to the resulting compounds of the method and their respective use.
专利号:US-8933181-B2 优先权日:2006-10-06 标题:Branched polymers and methods for their synthesis and use 发明人:MOURI HIROSHI; LUO STEVEN; KURASCH JESSICA; ROBERTSON CHRISTOPHER G; WARREN SANDRA 权利人:MOURI HIROSHI; LUO STEVEN; KURASCH JESSICA; ROBERTSON CHRISTOPHER G; WARREN SANDRA; BRIDGESTONE CORP 摘要:Branched polymers including multi-branched polymers, functionalized branched polymers, star-branched polymers, and dendigraft polymers. Methods for the synthesis of branched polymers and method for the use of branched polymers in tire components are also included.
专利号:US-7705159-B2 优先权日:2005-07-06 标题:Process for the preparation of letrozole 发明人:MACDONALD PETER LINDSAY; BIGATTI ETTORE; ROSSETTO PIERLUIGI; HAREL ZVI 权利人:SICOR INC 摘要:The invention provides a high-yield process for the preparation of letrozole having a high purity, without the need for removal of the 4-[1-(1,3,4-triazolyl)methyl]benzonitrile impurity at the intermediate stage. The invention also provides a process for the synthesis of letrozole in which formation of the impurity 4-[1-(1,3,4-triazolyl)methyl]benzonitrile during the first stage is minimized. In the process, a 4-(halomethyl)benzonitrile is reacted with a salt of 1H-1,2,4-triazole, reducing the formation of the impurity. Preferably, the preparation is conducted as a one-pot process.
专利号:WO-2024168123-A1 优先权日:2023-02-09 标 题 :Synthesis of core 2 o-sialyl lewis-x polysaccharides 发明人:CHAIKOF ELLIOT; DHAKAL BIBEK; MANDHAPATI APPI; ERADI PRADHEEP 权利人:BETH ISRAEL DEACONESS MEDICAL CT INC 摘要:Provided herein are methods and compounds useful in the preparation of Core 2 O -sialyl Lewis x polysaccharides including compounds of Formula (C).
专利号:US-12295961-B2 优先权日:2009-12-31 标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols 发明人:DHINGRA OM 权利人:MARIUS PHARMACEUTICALS INC 摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.